N-(4-(4-烷基哌嗪-1-基)苯基)苯甲酰胺类化合物的合成及构效关系研究作为毒蕈碱型乙酰胆碱受体亚型 1（M1）拮抗剂。
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
机构信息
Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
出版信息
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2174-7. doi: 10.1016/j.bmcl.2010.02.041. Epub 2010 Feb 13.
Abstract
This Letter describes the synthesis and SAR, developed through an iterative analog library approach, of a novel series of selective M(1) mAChR antagonists, based on an N-(4-(4-alkylpiperazin-1-yl)phenyl)benzamide scaffold for the potential treatment of Parkinson's disease, dystonia and other movement disorders. Compounds in this series possess M(1) antagonist IC(50)s in the 350 nM to >10 microM range with varying degrees of functional selectivity versus M(2)-M(5).
摘要
这封信描述了一种新型的选择性 M(1) mAChR 拮抗剂的合成和 SAR 研究，该拮抗剂是基于 N-(4-(4-烷基哌嗪-1-基)苯基)苯甲酰胺支架，为治疗帕金森病、肌张力障碍和其他运动障碍而开发的。该系列化合物具有 350 nM 至 >10 microM 的 M(1)拮抗剂 IC(50)，对 M(2)-M(5)具有不同程度的功能选择性。
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